quinolines

Summary

Top Publications

  1. ncbi Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity
    Sauveur Michel Maira
    Oncology Disease Area, Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH4002 Basel, Switzerland
    Mol Cancer Ther 7:1851-63. 2008
  2. ncbi NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations
    Violeta Serra
    Laboratory of Oncology Research, Medical Oncology Service, Vall d Hebron University Hospital, Barcelona, Spain
    Cancer Res 68:8022-30. 2008
  3. ncbi Effects of torcetrapib in patients at high risk for coronary events
    Philip J Barter
    Heart Research Institute, Camperdown, Sydney, NSW, Australia
    N Engl J Med 357:2109-22. 2007
  4. ncbi A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis
    Koen Andries
    Johnson and Johnson Pharmaceutical Research and Development, Turnhoutseweg 30, 2340 Beerse, Belgium
    Science 307:223-7. 2005
  5. pmc Dihydroartemisinin-piperaquine and artemether-lumefantrine for treating uncomplicated malaria in African children: a randomised, non-inferiority trial
    Quique Bassat
    Barcelona Centre for International Health Research CRESIB, Hospital Clinic, Institut d Investigacions Biomediques August Pi i Sunyer, Universitat de Barcelona, Barcelona, Spain
    PLoS ONE 4:e7871. 2009
  6. pmc Population pharmacokinetics and pharmacodynamics of piperaquine in children with uncomplicated falciparum malaria
    J Tarning
    Mahidol Oxford Tropical Medicine Research Unit, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand
    Clin Pharmacol Ther 91:497-505. 2012
  7. pmc The efficacy of the novel dual PI3-kinase/mTOR inhibitor NVP-BEZ235 compared with rapamycin in renal cell carcinoma
    Daniel C Cho
    Division of Hematology and Oncology, Beth Israel Deaconess Medical Center, Boston, Massachusetts 02215, USA
    Clin Cancer Res 16:3628-38. 2010
  8. ncbi Artemether-lumefantrine versus dihydroartemisinin-piperaquine for falciparum malaria: a longitudinal, randomized trial in young Ugandan children
    Emmanuel Arinaitwe
    Makerere University University of California San Francisco Research Collaboration, University of California, San Francisco 94143, USA
    Clin Infect Dis 49:1629-37. 2009
  9. pmc NVP-BEZ235, a novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor, elicits multifaceted antitumor activities in human gliomas
    Ta Jen Liu
    Department of Neuro Oncology, The University of Texas M D Anderson Cancer Center, Unit 431, 1515 Holcombe Boulevard, Houston, TX 77030
    Mol Cancer Ther 8:2204-10. 2009
  10. ncbi Activity of the novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 against T-cell acute lymphoblastic leukemia
    Francesca Chiarini
    Department of Human Anatomy, University of Bologna, Bologna, Italy
    Cancer Res 70:8097-107. 2010

Detail Information

Publications335 found, 100 shown here

  1. ncbi Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity
    Sauveur Michel Maira
    Oncology Disease Area, Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH4002 Basel, Switzerland
    Mol Cancer Ther 7:1851-63. 2008
    ..Collectively, the preclinical data show that NVP-BEZ235 is a potent dual PI3K/mTOR modulator with favorable pharmaceutical properties. NVP-BEZ235 is currently in phase I clinical trials...
  2. ncbi NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations
    Violeta Serra
    Laboratory of Oncology Research, Medical Oncology Service, Vall d Hebron University Hospital, Barcelona, Spain
    Cancer Res 68:8022-30. 2008
    ..In summary, NVP-BEZ235 inhibits the PI3K/mTOR axis and results in antiproliferative and antitumoral activity in cancer cells with both wild-type and mutated p110-alpha...
  3. ncbi Effects of torcetrapib in patients at high risk for coronary events
    Philip J Barter
    Heart Research Institute, Camperdown, Sydney, NSW, Australia
    N Engl J Med 357:2109-22. 2007
    ..We investigated whether torcetrapib, a potent CETP inhibitor, might reduce major cardiovascular events. The trial was terminated prematurely because of an increased risk of death and cardiac events in patients receiving torcetrapib...
  4. ncbi A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis
    Koen Andries
    Johnson and Johnson Pharmaceutical Research and Development, Turnhoutseweg 30, 2340 Beerse, Belgium
    Science 307:223-7. 2005
    ..Plasma levels associated with efficacy in mice were well tolerated in healthy human volunteers. Mutants selected in vitro suggest that the drug targets the proton pump of adenosine triphosphate (ATP) synthase...
  5. pmc Dihydroartemisinin-piperaquine and artemether-lumefantrine for treating uncomplicated malaria in African children: a randomised, non-inferiority trial
    Quique Bassat
    Barcelona Centre for International Health Research CRESIB, Hospital Clinic, Institut d Investigacions Biomediques August Pi i Sunyer, Universitat de Barcelona, Barcelona, Spain
    PLoS ONE 4:e7871. 2009
    ..Dihydroartemisinin-piperaquine (DHA-PQP) is a promising fixed-dose ACT with limited information on its safety and efficacy in African children...
  6. pmc Population pharmacokinetics and pharmacodynamics of piperaquine in children with uncomplicated falciparum malaria
    J Tarning
    Mahidol Oxford Tropical Medicine Research Unit, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand
    Clin Pharmacol Ther 91:497-505. 2012
    ..025) but had significantly lower day 7 piperaquine concentrations (P = 0.024) and total piperaquine exposures (P = 0.021), suggesting that an increased dose regimen for young children should be evaluated...
  7. pmc The efficacy of the novel dual PI3-kinase/mTOR inhibitor NVP-BEZ235 compared with rapamycin in renal cell carcinoma
    Daniel C Cho
    Division of Hematology and Oncology, Beth Israel Deaconess Medical Center, Boston, Massachusetts 02215, USA
    Clin Cancer Res 16:3628-38. 2010
    ....
  8. ncbi Artemether-lumefantrine versus dihydroartemisinin-piperaquine for falciparum malaria: a longitudinal, randomized trial in young Ugandan children
    Emmanuel Arinaitwe
    Makerere University University of California San Francisco Research Collaboration, University of California, San Francisco 94143, USA
    Clin Infect Dis 49:1629-37. 2009
    ..However, which therapies are optimal is a matter of debate. We aimed to compare the short- and longer-term efficacy of 2 leading therapies in a cohort of young Ugandan children...
  9. pmc NVP-BEZ235, a novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor, elicits multifaceted antitumor activities in human gliomas
    Ta Jen Liu
    Department of Neuro Oncology, The University of Texas M D Anderson Cancer Center, Unit 431, 1515 Holcombe Boulevard, Houston, TX 77030
    Mol Cancer Ther 8:2204-10. 2009
    ..These results warrant further development of NVP-BEZ235 for clinical trials for human gliomas or other advanced cancers with altered PI3K/Akt/mTOR signaling...
  10. ncbi Activity of the novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 against T-cell acute lymphoblastic leukemia
    Francesca Chiarini
    Department of Human Anatomy, University of Bologna, Bologna, Italy
    Cancer Res 70:8097-107. 2010
    ....
  11. pmc Dual targeting of phosphoinositide 3-kinase and mammalian target of rapamycin using NVP-BEZ235 as a novel therapeutic approach in human ovarian carcinoma
    Chintda Santiskulvong
    Division of Gynecologic Oncology, Departments of Obstetrics and Gynecology, UCLA David Geffen School of Medicine, Los Angeles, CA 90095 1740, USA
    Clin Cancer Res 17:2373-84. 2011
    ..This study evaluates the effect of dual PI3K and mTOR inhibition using NVP-BEZ235 in preclinical models of ovarian cancer as a potential novel therapeutic strategy...
  12. ncbi Inhibition of metastasis in a castration resistant prostate cancer model by the quinoline-3-carboxamide tasquinimod (ABR-215050)
    Karin Jennbacken
    Sahlgrenska Cancer Center, Department of Urology, Institute of Clinical Sciences, Sahlgrenska Academy at University of Gothenburg, Box 425, 40530 Goteborg, Sweden
    Prostate 72:913-24. 2012
    ..Its mechanism of action is not fully elucidated, but previous studies show anti-angiogenic effects and strong interaction with the S100A9 protein...
  13. pmc Declining responsiveness of Plasmodium falciparum infections to artemisinin-based combination treatments on the Kenyan coast
    Steffen Borrmann
    Kenya Medical Research Institute Wellcome Trust Research Programme, Kilifi, Kenya
    PLoS ONE 6:e26005. 2011
    ..The emergence of artemisinin-resistant P. falciparum malaria in South-East Asia highlights the need for continued global surveillance of the efficacy of artemisinin-based combination therapies...
  14. ncbi Dual inhibition of PI3K and mTORC1/2 signaling by NVP-BEZ235 as a new therapeutic strategy for acute myeloid leukemia
    Nicolas Chapuis
    Institut Cochin, Universite Paris Descartes, CNRS UMR8104 INSERM U1016 Service d Hématologie Biologique, Hopital Cochin, AP HP, Paris, France
    Clin Cancer Res 16:5424-35. 2010
    ..We therefore tested, in this study, the antileukemic activity of the dual PI3K/mTOR ATP-competitive inhibitor NVP-BEZ235 compound (Novartis)...
  15. ncbi Efficacy and safety of dihydroartemisinin-piperaquine for treatment of uncomplicated Plasmodium falciparum malaria in endemic countries: meta-analysis of randomised controlled studies
    Cho Naing
    School of Postgraduate Studies and Research, International Medical University, Kuala Lumpur 57000, Malaysia
    Trans R Soc Trop Med Hyg 107:65-73. 2013
    ..The better safety profile of DP and once-daily dosage improves adherence and its fixed co-formulation ensures that both drugs are taken together. Our conclusion is that DP has the potential to become a first-line antimalarial drug...
  16. pmc S6K1 and 4E-BP1 are independent regulated and control cellular growth in bladder cancer
    Roman Nawroth
    Department of Urology, Klinikum rechts der Isar der Technischen Universitat Munchen, Munich, Germany
    PLoS ONE 6:e27509. 2011
    ..Our data suggest that 4E-BP1 is a potential new target molecule and stratification marker for anti cancer therapy in UC and support the consideration of a multi-targeting approach against PI3K, mTORC1/2 and MAPK...
  17. ncbi Diarylquinolines are bactericidal for dormant mycobacteria as a result of disturbed ATP homeostasis
    Anil Koul
    Departments of Antimicrobial Research and Functional Genomics, Johnson and Johnson, Turnhoutseweg 30, B 2340 Beerse, Belgium
    J Biol Chem 283:25273-80. 2008
    ....
  18. pmc Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235
    Pieter J A Eichhorn
    Medical Oncology Program, Vall d Hebron Institut de Oncologia, Barcelona, Spain
    Cancer Res 68:9221-30. 2008
    ..Our data show that deregulation of the PI3K pathway, either through loss-of-function mutations in PTEN or dominant activating mutations in PIK3CA, leads to lapatinib resistance, which can be effectively reversed by NVP-BEZ235...
  19. ncbi Crosstalk between the PI3K/mTOR and MEK/ERK pathways involved in the maintenance of self-renewal and tumorigenicity of glioblastoma stem-like cells
    Jun Sunayama
    Department of Molecular Cancer Science Yamagata University School of Medicine, Yamagata, Japan
    Stem Cells 28:1930-9. 2010
    ..Thus, combinational disruption of these pathways would be a rational and effective strategy in the treatment of glioblastoma...
  20. ncbi Substitution of moxifloxacin for isoniazid during intensive phase treatment of pulmonary tuberculosis
    Susan E Dorman
    Johns Hopkins University Center for Tuberculosis Research, Baltimore, Maryland 21231, USA
    Am J Respir Crit Care Med 180:273-80. 2009
    ..Moxifloxacin has potent activity against Mycobacterium tuberculosis in vitro and in a mouse model of antituberculosis (TB) chemotherapy, but data regarding its activity in humans are limited...
  21. ncbi ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity
    Neru Munshi
    Boston Biomedical, Inc, Norwood, Massachusetts, USA
    Mol Cancer Ther 9:1544-53. 2010
    ..Cumulatively, these data suggest that ARQ 197, currently in phase II clinical trials, is a promising agent for targeting cancers in which c-Met-driven signaling is important for their survival and proliferation...
  22. pmc The dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer
    Jatin Roper
    Division of Gastroenterology, Department of Medicine, Tufts Medical Center, Boston, Massachusetts, United States of America
    PLoS ONE 6:e25132. 2011
    ..To examine the in vitro and in vivo efficacy of the dual PI3K/mTOR inhibitor NVP-BEZ235 in treatment of PIK3CA wild-type colorectal cancer (CRC)...
  23. pmc Increased AKT S473 phosphorylation after mTORC1 inhibition is rictor dependent and does not predict tumor cell response to PI3K/mTOR inhibition
    Madlaina Breuleux
    Novartis Pharma AG, Novartis Institutes for BioMedical Research, Oncology, Basel, Switzerland
    Mol Cancer Ther 8:742-53. 2009
    ..However, reduced cell viability could not be predicted from biochemical or cellular responses to mTORC1 inhibitors. These data could have implications for the clinical application of phosphatidylinositol 3-kinase/mTOR inhibitors...
  24. ncbi Phase I trial of a selective c-MET inhibitor ARQ 197 incorporating proof of mechanism pharmacodynamic studies
    Timothy A Yap
    Royal Marsden National Health Service Foundation Trust, The Institute of Cancer Research, Sutton, Surrey, UK
    J Clin Oncol 29:1271-9. 2011
    ..A phase I trial of ARQ 197 was conducted to assess safety, tolerability, and target inhibition, including intratumoral c-MET signaling, apoptosis, and angiogenesis...
  25. ncbi Phase II randomized, double-blind, placebo-controlled study of tasquinimod in men with minimally symptomatic metastatic castrate-resistant prostate cancer
    Roberto Pili
    Roswell Park Cancer Institute, Buffalo, NY 14263 0001, USA
    J Clin Oncol 29:4022-8. 2011
    ..The activity of the novel antitumor agent tasquinimod (TASQ) with S100A9 as a molecular target was investigated in men with metastatic castration-resistant prostate cancer (CRPC) and minimal symptoms...
  26. ncbi Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells
    L L Remsing Rix
    Center for Molecular Medicine of the Austrian Academy of Sciences, Vienna, Austria
    Leukemia 23:477-85. 2009
    ..Finally, bosutinib is the first kinase inhibitor shown to target CAMK2G, recently implicated in myeloid leukemia cell proliferation...
  27. ncbi The diarylquinoline TMC207 for multidrug-resistant tuberculosis
    Andreas H Diacon
    Centre for Clinical Tuberculosis Research, the Department of Science and Technology, Faculty of Health Sciences, University of Stellenbosch, Tygerberg, all in South Africa
    N Engl J Med 360:2397-405. 2009
    ..TMC207 potently inhibits drug-sensitive and drug-resistant Mycobacterium tuberculosis in vitro and shows bactericidal activity in patients who have drug-susceptible pulmonary tuberculosis...
  28. ncbi Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties
    T M Caserta
    Department of Physiology and Biophysics, Wright State University School of Medicine, Dayton, Ohio 45435, USA
    Apoptosis 8:345-52. 2003
    ..Our data indicate that the specificity, effectiveness, and reduced toxicity of caspase inhibitors can be significantly enhanced using carboxyterminal o-phenoxy groups and may have important uses in vivo...
  29. pmc Dual phosphoinositide 3-kinase/mammalian target of rapamycin blockade is an effective radiosensitizing strategy for the treatment of non-small cell lung cancer harboring K-RAS mutations
    Georgia Konstantinidou
    Division of Hematology and Oncology, Simmons Comprehensive Cancer Center, and Hamon Center for Therapeutic Oncology Research, Department of Pathology, University of Texas Southwestern Medical Center, Dallas, Texas TX 75390, USA
    Cancer Res 69:7644-52. 2009
    ..These findings may have general applicability in cancer therapy, because aberrant activation of PI3K occurs frequently in human cancer...
  30. ncbi NVP-BEZ235 as a new therapeutic option for sarcomas
    Maria C Manara
    Laboratorio di Ricerca Oncologica, Istituto Ortopedico Rizzoli, Bologna, Italy
    Clin Cancer Res 16:530-40. 2010
    ..To evaluate the in vitro and in vivo effects of NVP-BEZ235, a dual pan-phosphoinositide 3-kinase-mammalian target of rapamycin inhibitor in the three most common musculoskeletal tumors (osteosarcoma, Ewing's sarcoma, and rhabdomyosarcoma)...
  31. pmc Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells
    Saskia M Brachmann
    Novartis Institutes for BioMedical Research, Oncology Disease Area, CH 4002 Basel, Switzerland
    Proc Natl Acad Sci U S A 106:22299-304. 2009
    ..Overall, this study will provide guidance for patient stratification for forthcoming breast cancer phase II trials for NVP-BEZ235...
  32. pmc Pleiotropic effects of pitavastatin
    Jean Davignon
    Hyperlipidemia and Atherosclerosis Research Group, Clinical Research Institute of Montréal IRCM and University of Montréal, QC, Canada
    Br J Clin Pharmacol 73:518-35. 2012
    ..It is concluded that the diverse pleiotropic actions of pitavastatin may contribute to reducing cardiovascular morbidity and mortality beyond that achieved through LDL-C reduction...
  33. pmc Safety and efficacy of dihydroartemisinin-piperaquine versus artemether-lumefantrine in the treatment of uncomplicated Plasmodium falciparum malaria in Zambian children
    Michael Nambozi
    Department of Clinical Sciences, Tropical Disease Research Center, P, O Box 71769, Ndola Zambia
    Malar J 10:50. 2011
    ..In 2002, the first-line treatment for uncomplicated malaria was changed to artemether-lumefantrine (AL) that has proved to be highly efficacious against multidrug resistant Plasmodium falciparum...
  34. ncbi A trial of combination antimalarial therapies in children from Papua New Guinea
    Harin A Karunajeewa
    School of Medicine and Pharmacology, University of Western Australia, Crawley, WA, Australia
    N Engl J Med 359:2545-57. 2008
    ..Malaria control is difficult where there is intense year-round transmission of multiple plasmodium species, such as in Papua New Guinea...
  35. ncbi G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17beta-estradiol and selective GPR30 ligand G-1 in ovarian cancer cells
    Lidia Albanito
    Departments of Pharmaco Biology and Cell Biology, University of Calabria, 87030 Rende Cosenza, Italy
    Cancer Res 67:1859-66. 2007
    ....
  36. pmc Population pharmacokinetics of dihydroartemisinin and piperaquine in pregnant and nonpregnant women with uncomplicated malaria
    Joel Tarning
    Mahidol Oxford Tropical Medicine Research Unit, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand
    Antimicrob Agents Chemother 56:1997-2007. 2012
    ..The clinical impact of these pharmacokinetic findings in pregnant women with uncomplicated malaria needs to be evaluated in larger series...
  37. pmc Differential induction of apoptosis in HER2 and EGFR addicted cancers following PI3K inhibition
    Anthony C Faber
    Massachusetts General Hospital Cancer Center, Harvard Medical School, Charlestown, MA 02129, USA
    Proc Natl Acad Sci U S A 106:19503-8. 2009
    ..These data indicate simultaneous inhibition of PI3K-mTOR and MEK signaling is an effective strategy for treating EGFR mutant lung cancers, including those with acquired resistance to EGFR TKIs...
  38. ncbi The novel orally bioavailable inhibitor of phosphoinositol-3-kinase and mammalian target of rapamycin, NVP-BEZ235, inhibits growth and proliferation in multiple myeloma
    Philipp Baumann
    Department of Hematology and Oncology Medizinische Klinik Innenstadt, Klinikum der Universitat Munchen, Germany
    Exp Cell Res 315:485-97. 2009
    ..Taken together, inhibition of PI3 kinase/mTOR by NVP-BEZ235 is highly effective and NVP-BEZ235 represents a potential new candidate for targeted therapy in multiple myeloma...
  39. ncbi In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells
    Miriam Puttini
    Department of Clinical Medicine, S Gerardo Hospital University of Milano Bicocca, Monza, Italy
    Cancer Res 66:11314-22. 2006
    ..Modeling considerations attribute the superior activity of SKI-606 to its ability to bind a conformation of Bcr-Abl different from imatinib...
  40. pmc Safety and efficacy of dihydroartemisinin-piperaquine in falciparum malaria: a prospective multi-centre individual patient data analysis
    Julien Zwang
    Shoklo Malaria Research Unit, Mae Sot, Thailand
    PLoS ONE 4:e6358. 2009
    ..Comparator drugs were mefloquine-artesunate (MAS3) in Thailand, Myanmar, Laos and Cambodia; artemether-lumefantrine in Uganda; and amodiaquine+sulfadoxine-pyrimethamine and artesunate+amodiaquine in Rwanda...
  41. pmc Preferential binding of a G-quadruplex ligand to human chromosome ends
    Christine Granotier
    LRP, DRR, CEA 92265, Fontenay aux Roses, France
    Nucleic Acids Res 33:4182-90. 2005
    ..They support the hypothesis that G-quadruplex ligands induce and/or stabilize G-quadruplex structures at telomeres of human cells...
  42. ncbi Phase I dose-escalation study and biomarker analysis of E7080 in patients with advanced solid tumors
    Kazuhiko Yamada
    Department of Internal Medicine, National Cancer Center Hospital, Tokyo, Japan
    Clin Cancer Res 17:2528-37. 2011
    ..This Phase I study investigated maximum tolerated dose (MTD), dose-limiting toxicity (DLT), pharmacokinetics (PK), pharmacodynamics (PD), and efficacy in patients with advanced solid tumors...
  43. pmc Tasquinimod (ABR-215050), a quinoline-3-carboxamide anti-angiogenic agent, modulates the expression of thrombospondin-1 in human prostate tumors
    Anders Olsson
    Active Biotech AB, Box 724, 22007 Lund, Sweden
    Mol Cancer 9:107. 2010
    ..The array data were validated by real-time semiquantitative reversed transcriptase polymerase chain reaction (sqRT-PCR) and protein expression techniques...
  44. ncbi Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo
    Kwang Yu Chang
    Institute of Clinical Medicine, Department of Cell Biology and Anatomy, College of Medicine, National Cheng Kung University, Tainan, Taiwan, Republic of China
    Clin Cancer Res 17:7116-26. 2011
    ..To develop a new treatment, we investigated the effect of a novel dual PI3K/mTOR inhibitor, NVP-BGT226 (BGT226), in head and neck cancer cells...
  45. ncbi A phase I dose-escalation study of Tivantinib (ARQ 197) in adult patients with metastatic solid tumors
    Lee S Rosen
    UCLA Division of Hematology Oncology, Los Angeles, CA 90404, USA
    Clin Cancer Res 17:7754-64. 2011
    ..This open-label, phase I, dose-escalation study evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of tivantinib in patients with advanced or metastatic solid tumors refractory to standard therapy...
  46. pmc Tasquinimod prevents the angiogenic rebound induced by fractionated radiation resulting in an enhanced therapeutic response of prostate cancer xenografts
    Susan L Dalrymple
    Department of Oncology, The Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, The Johns Hopkins University School of Medicine, Baltimore, Maryland, USA
    Prostate 72:638-48. 2012
    ....
  47. pmc Randomized, open-label trial of primaquine against vivax malaria relapse in Indonesia
    Inge Sutanto
    Faculty of Medicine, University of Indonesia, Jakarta, Indonesia
    Antimicrob Agents Chemother 57:1128-35. 2013
    ..Antirelapse therapy with primaquine begun a month after treatment of the acute attack with dihydroartemisinin-piperaquine proved safe and highly efficacious against relapse by P. vivax acquired in Papua, Indonesia...
  48. pmc Activity of a novel, dual PI3-kinase/mTor inhibitor NVP-BEZ235 against primary human pancreatic cancers grown as orthotopic xenografts
    P Cao
    Division of Applied Molecular Oncology, Department of Medical Oncology and Hematology, Ontario Cancer Institute Princess Margaret Hospital, University of Toronto, Ontario, Canada
    Br J Cancer 100:1267-76. 2009
    ..These results predict that agents targeting the PI3K/Akt/mTor pathway might have anticancer activity in pancreatic cancer patients, and support the testing of combination studies involving chemotherapy or other molecular targeted agents...
  49. pmc A phase I study of E7080, a multitargeted tyrosine kinase inhibitor, in patients with advanced solid tumours
    D S Boss
    Division of Medical Oncology, Department of Clinical Pharmacology, The Netherlands Cancer Institute, Plesmanlaan 121, Amsterdam, The Netherlands
    Br J Cancer 106:1598-604. 2012
    ....
  50. ncbi MvfR, a key Pseudomonas aeruginosa pathogenicity LTTR-class regulatory protein, has dual ligands
    Gaoping Xiao
    Department of Surgery, Harvard Medical School, Massachusetts General Hospital, USA
    Mol Microbiol 62:1689-99. 2006
    ..These results uncover a novel biological role for HHQ; and provide novel insights on MvfR activation that may aid in the development of therapies that prevent or treat P. aeruginosa infections in humans...
  51. ncbi Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases
    Fawn Qian
    Exelixis, Inc, South San Francisco, California 94083, USA
    Cancer Res 69:8009-16. 2009
    ..Collectively, these data indicate that EXEL-2880 may prevent tumor growth through a direct effect on tumor cell proliferation and by inhibition of invasion and angiogenesis mediated by HGF and VEGF receptors...
  52. ncbi Effect of intensive statin therapy on regression of coronary atherosclerosis in patients with acute coronary syndrome: a multicenter randomized trial evaluated by volumetric intravascular ultrasound using pitavastatin versus atorvastatin (JAPAN-ACS [Japan
    Takafumi Hiro
    Division of Cardiology, Department of Medicine and Clinical Science, Yamaguchi University Graduate School of Medicine, Ube, Japan
    J Am Coll Cardiol 54:293-302. 2009
    ....
  53. pmc Vertical targeting of the phosphatidylinositol-3 kinase pathway as a strategy for treating melanoma
    Saadia A Aziz
    Department of Pathology, Yale University School of Medicine, Yale Cancer Center, New Haven, Connecticut 06510, USA
    Clin Cancer Res 16:6029-39. 2010
    ..Phosphatidylinositol-3 kinase (PI3K) is an important target in melanoma; however, activity of PI3K inhibitors (PI3KI) is limited. Our purpose was to assess mTOR as a cotarget for PI3K...
  54. ncbi Pharmacokinetics of the antimalarial drug piperaquine in healthy Vietnamese subjects
    Trong Chinh Nguyen
    Department of Infectious Diseases, Central Military Hospital 108, Hanoi, Vietnam
    Am J Trop Med Hyg 79:620-3. 2008
    ..Piperaquine AUC was proportional to the two doses tested and a moderate-fat meal enhanced the bioavailability of piperaquine by 41%, which should improve the therapeutic efficacy of this drug...
  55. ncbi Antimyeloma activity of the orally bioavailable dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235
    Douglas W McMillin
    Jerome Lipper Multiple Myeloma Center, Department of Medical Oncology, Dana Farber Cancer Institute, Boston, Massachusetts 02115, USA
    Cancer Res 69:5835-42. 2009
    ..g., dexamethasone and doxorubicin) or novel (e.g., bortezomib) anti-MM agents showed lack of antagonism. These results indicate that BEZ235 merits clinical testing, alone and in combination with other agents, in MM...
  56. ncbi A phase I study of foretinib, a multi-targeted inhibitor of c-Met and vascular endothelial growth factor receptor 2
    Joseph Paul Eder
    Early Drug Development Center, Department of Medical Oncology, Dana Farber Cancer Institute and Department of Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, Massachusetts, USA
    Clin Cancer Res 16:3507-16. 2010
    ..Secondary objectives included evaluation of plasma pharmacokinetics, long-term safety after repeated administration, preliminary antitumor activity, and pharmacodynamic activity...
  57. pmc Adverse pregnancy outcomes in an area where multidrug-resistant plasmodium vivax and Plasmodium falciparum infections are endemic
    Jeanne Rini Poespoprodjo
    District Health Authority, School of Health Research National Institute of Health Research and Development Malaria Research Program, Indonesia
    Clin Infect Dis 46:1374-81. 2008
    ..Plasmodium falciparum infection exerts a considerable burden on pregnant women, but less is known about the adverse consequences of Plasmodium vivax infection...
  58. ncbi Safety and efficacy of bosutinib (SKI-606) in chronic phase Philadelphia chromosome-positive chronic myeloid leukemia patients with resistance or intolerance to imatinib
    Jorge E Cortes
    M D Anderson Cancer Center, Houston, TX, USA
    Blood 118:4567-76. 2011
    ..These data suggest bosutinib is effective and tolerable in patients with chronic phase imatinib-resistant or imatinib-intolerant CML. This trial was registered at http://www.clinicaltrials.gov as NCT00261846...
  59. ncbi Effects of cysteinyl leukotrienes in small human bronchus and antagonist activity of montelukast and its metabolites
    H Mechiche
    Laboratory of Pharmacology, EA 2070, Faculty of Medicine, Reims, France
    Clin Exp Allergy 33:887-94. 2003
    ..Montelukast (MK), a specific CysLT1 receptor antagonist, is metabolized in two main hydroxylated metabolites (termed M5 and M6, respectively)...
  60. ncbi A role for cysteinyl leukotrienes in airway remodeling in a mouse asthma model
    William R Henderson
    Departments of Medicine and Pathology, University of Washington, Seattle, Washington 98195 6523, USA
    Am J Respir Crit Care Med 165:108-16. 2002
    ..These data suggest an important role for cysteinyl leukotrienes in the pathogenesis of chronic allergic airway inflammation with fibrosis...
  61. ncbi Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors
    Romina Marone
    Department of Biomedicine, University of Basel, Mattenstrasse 28, CH 4058 Basel, Switzerland
    Mol Cancer Res 7:601-13. 2009
    ..Based on the above results, NVP-BEZ235, which has entered phase I/II clinical trials in patients with advanced solid tumors, has a potential in metastatic melanoma therapy...
  62. pmc Pharmacokinetics, safety, and tolerability of ascending single doses of moxifloxacin, a new 8-methoxy quinolone, administered to healthy subjects
    H Stass
    Pharma Research Center, Institute of Clinical Pharmacology, Bayer AG, 42096 Wuppertal, Germany
    Antimicrob Agents Chemother 42:2060-5. 1998
    ..The pharmacokinetic parameters derived from compartmental and noncompartmental analyses were in good agreement. The kinetics could be described best by fitting the data to a two-compartment body model...
  63. ncbi Inhibition profiles of phosphatidylinositol 3-kinase inhibitors against PI3K superfamily and human cancer cell line panel JFCR39
    Dexin Kong
    Division of Molecular Pharmacology, Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, 3 10 6, Ariake, Koto ku, Tokyo 135 8550, Japan
    Eur J Cancer 46:1111-21. 2010
    ..The biological implication of the difference in molecular target specificity of these PI3K inhibitors is under investigation...
  64. pmc The combination of RAD001 and NVP-BEZ235 exerts synergistic anticancer activity against non-small cell lung cancer in vitro and in vivo
    Cheng Xiong Xu
    Department of Hematology and Medical Oncology, Emory University School of Medicine and Winship Cancer Institute, Atlanta, Georgia, United States of America
    PLoS ONE 6:e20899. 2011
    ..Taken together, our results suggest that the combination of RAD001 and BEZ235 is a novel strategy for cancer therapy...
  65. ncbi Synergistic action of a RAF inhibitor and a dual PI3K/mTOR inhibitor in thyroid cancer
    Ning Jin
    Cancer Biology Division, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Baltimore, Maryland, USA
    Clin Cancer Res 17:6482-9. 2011
    ..We tested a novel drug combination targeting RAF, phosphoinositide 3-kinase (PI3K), and mTOR, plus VEGFR2 and RET, in thyroid cancer preclinical models with defined genetic backgrounds...
  66. pmc Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand
    J Tarning
    Department of Pharmacology, Sahlgrenska Academy at Goteborg University, Goteborg, Sweden
    Antimicrob Agents Chemother 52:1052-61. 2008
    ..Our data lend further support to a simplified once-daily treatment regimen to improve treatment adherence and efficacy and indicate that weight-adjusted piperaquine doses in children may need to be higher than in adults...
  67. pmc Population pharmacokinetics of piperaquine in adults and children with uncomplicated falciparum or vivax malaria
    Te Yu Hung
    Medicine Unit Fremantle Hospital and Pharmacology Unit Queen Elizabeth 2 Medical Centre, School of Medicine and Pharmacology, University of Western Australia, Crawley, Western Australia, Australia
    Br J Clin Pharmacol 57:253-62. 2004
    ..To study the population pharmacokinetics of piperaquine after co-administration with dihydroartemisinin in uncomplicated malaria...
  68. pmc An open-label, randomised study of dihydroartemisinin-piperaquine versus artesunate-mefloquine for falciparum malaria in Asia
    Neena Valecha
    National Institute of Malaria Research, Delhi, India
    PLoS ONE 5:e11880. 2010
    ..The aim of this study was to show non-inferiority of DHA/PQP vs. artesunate-mefloquine (AS+MQ) in Asia...
  69. pmc A randomized trial to monitor the efficacy and effectiveness by QT-NASBA of artemether-lumefantrine versus dihydroartemisinin-piperaquine for treatment and transmission control of uncomplicated Plasmodium falciparum malaria in western Kenya
    Petra F Mens
    Koninklijk Instituut voor de Tropen KIT Royal Tropical Institute, KIT Biomedical Research, Amsterdam, The Netherlands
    Malar J 7:237. 2008
    ....
  70. ncbi Piperaquine: a resurgent antimalarial drug
    Timothy M E Davis
    Medicine Unit Fremantle and Pharmacology Unit Nedlands, School of Medicine and Pharmacology, University of Western Australia, Crawley, Western Australia, Australia
    Drugs 65:75-87. 2005
    ..The tolerability, efficacy, pharmacokinetic profile and low cost of piperaquine make it a promising partner drug for use as part of an ACT...
  71. ncbi Randomized head-to-head comparison of pitavastatin, atorvastatin, and rosuvastatin for safety and efficacy (quantity and quality of LDL): the PATROL trial
    Keijiro Saku
    Department of Cardiology, Fukuoka University School of Medicine, Fukuoka, Japan
    Circ J 75:1493-505. 2011
    ..This is the first prospective randomized multi-center trial to compare these strong statins (UMIN Registration No: 000000586)...
  72. ncbi Oral montelukast in acute asthma exacerbations: a randomised, double-blind, placebo-controlled trial
    Crichton F Ramsay
    Department of Respiratory Medicine, Norfolk and Norwich University Hospital, Norwich, UK
    Thorax 66:7-11. 2011
    ..Although leukotriene receptor antagonists have an established role in the management of patients with chronic asthma, their efficacy in an acute asthma exacerbation is not fully known...
  73. ncbi Comparative long-term efficacy and tolerability of pitavastatin 4 mg and atorvastatin 20-40 mg in patients with type 2 diabetes mellitus and combined (mixed) dyslipidaemia
    J Gumprecht
    Department of Internal Diseases, Diabetology and Nephrology, Medical University of Silesia, Zabrze, Poland
    Diabetes Obes Metab 13:1047-55. 2011
    ..To compare the long-term efficacy and safety of pitavastatin with atorvastatin in patients with type 2 diabetes and combined (mixed) dyslipidaemia...
  74. pmc Effect of single nucleotide polymorphisms in cytochrome P450 isoenzyme and N-acetyltransferase 2 genes on the metabolism of artemisinin-based combination therapies in malaria patients from Cambodia and Tanzania
    Eva Maria Staehli Hodel
    Swiss Tropical and Public Health Institute, University of Basel, Basel, Switzerland
    Antimicrob Agents Chemother 57:950-8. 2013
    ..data need not be included in appropriate first-line treatments with the current artemisinin derivatives and quinolines for uncomplicated malaria in specific populations...
  75. pmc Synthesis and in vivo evaluation of [11C]tariquidar, a positron emission tomography radiotracer based on a third-generation P-glycoprotein inhibitor
    Florian Bauer
    Department of Medicinal Chemistry, University of Vienna, Austria
    Bioorg Med Chem 18:5489-97. 2010
    ..Our data suggest that [(11)C]-1 interacts specifically with P-gp and BCRP in the BBB. However, further investigations are needed to assess if [(11)C]-1 behaves in vivo as a transported or a non-transported inhibitor...
  76. pmc Pulsed moxifloxacin for the prevention of exacerbations of chronic obstructive pulmonary disease: a randomized controlled trial
    Sanjay Sethi
    Division of Pulmonary, Critical Care and Sleep Medicine, University of Buffalo, State University of New York, Buffalo, NY, USA
    Respir Res 11:10. 2010
    ..This proof-of-concept study evaluates whether intermittent pulsed moxifloxacin treatment could reduce the frequency of these exacerbations...
  77. ncbi Vaccine adjuvant activity of 3M-052: an imidazoquinoline designed for local activity without systemic cytokine induction
    Dmitri Smirnov
    3M Drug Delivery Systems, 3M Center, St Paul, MN 55144, USA
    Vaccine 29:5434-42. 2011
    ..Given subcutaneously, 3M-052 drives a strong Th1 response to hemagglutinin and serum neutralization of viable H1N1 A/Puerto Rico/8/34 virus in the absence of circulating TNFα or the induction of Th1 cytokines...
  78. ncbi Residual antimalarial concentrations before treatment in patients with malaria from Cambodia: indication of drug pressure
    Eva Maria Hodel
    Swiss Tropical Institute, Basel, Switzerland
    J Infect Dis 202:1088-94. 2010
    ..There is a highly diverse market for antimalarials in this area, and improved knowledge of drug pressure would be useful to target interventions aimed at reducing inappropriate drug use...
  79. ncbi Antitumor activity and safety of tivozanib (AV-951) in a phase II randomized discontinuation trial in patients with renal cell carcinoma
    Dmitry A Nosov
    Blokhin Oncology Research Center, Russia
    J Clin Oncol 30:1678-85. 2012
    ..The antitumor activity and safety of tivozanib, which is a potent and selective vascular endothelial growth factor receptor-1, -2, and -3 inhibitor, was assessed in patients with advanced/metastatic renal cell carcinoma (RCC)...
  80. ncbi Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma
    Philipp Baumann
    Abteilung Hämatologie und Onkologie, Medizinische Klinik, Campus Innenstadt, Klinikum der Universitat Munchen, Munchen, Germany
    Anticancer Drugs 23:131-8. 2012
    ..Overall, inhibition of phosphoinositol-3-kinase/mammalian target of rapamycin by NVP-BGT226 is highly effective, and NVP-BGT226 represents a potential new candidate for targeted therapy in multiple myeloma...
  81. ncbi Adding moxifloxacin is associated with a shorter time to culture conversion in pulmonary tuberculosis
    J Y Wang
    Department of Internal Medicine, National Taiwan University College of Medicine and Hospital, Taipei, Taiwan
    Int J Tuberc Lung Dis 14:65-71. 2010
    ..To investigate whether adding moxifloxacin (MXF) to the standard anti-tuberculosis regimen can shorten the time to sputum culture conversion in pulmonary tuberculosis (PTB)...
  82. ncbi Safety profile of the respiratory fluoroquinolone moxifloxacin: comparison with other fluoroquinolones and other antibacterial classes
    Francoise Van Bambeke
    Unité de pharmacologie cellulaire et moléculaire and Centre de Pharmacie Clinique, Louvain Drug Research Institute, Universite Catholique de Louvain, Brussels, Belgium
    Drug Saf 32:359-78. 2009
    ....
  83. pmc New susceptibility breakpoints for first-line antituberculosis drugs based on antimicrobial pharmacokinetic/pharmacodynamic science and population pharmacokinetic variability
    Tawanda Gumbo
    Division of Infectious Diseases, UT Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390 9113, USA
    Antimicrob Agents Chemother 54:1484-91. 2010
    ..With the proposed breakpoints, the rates of multidrug-resistant tuberculosis could become 4-fold higher than currently assumed...
  84. ncbi Pitavastatin induces PON1 expression through p44/42 mitogen-activated protein kinase signaling cascade in Huh7 cells
    Kaoru Arii
    Department of Endocrinology, Metabolism and Nephrology, Kochi Medical School, Kochi University, Kohasu, Oko cho, Nankoku, Kochi 783 8505, Japan
    Atherosclerosis 202:439-45. 2009
    ..Furthermore, we speculate that pitavastatin affects both the phosphorylation of SREBP-2 and the Sp1 binding to PON1 DNA through the activation of p44/42 MAP kinase signaling cascade...
  85. ncbi Pitavastatin improves plasma pentraxin 3 and arterial stiffness in atherosclerotic patients with hypercholesterolemia
    Hiroyuki Ohbayashi
    Department of Internal Medicine, JA Gifu Tohno Kousei Hospital, Gifu, Japan
    J Atheroscler Thromb 16:490-500. 2009
    ..To investigate the effect of pitavastatin on asymptomatic atherosclerosis in patients with hypercholesterolemia...
  86. pmc ATR contributes to telomere maintenance in human cells
    Gaëlle Pennarun
    CEA DSV iRCM SCSR, Laboratoire de Radiopathologie, INSERM Université Paris VII U967, 92265 Fontenay aux Roses, France
    Nucleic Acids Res 38:2955-63. 2010
    ..Altogether, these data reveal that ATR plays a critical role in telomere maintenance during and/or after telomere replication in human cells...
  87. pmc Highly effective therapy for maternal malaria associated with a lower risk of vertical transmission
    J R Poespoprodjo
    District Health Authority, Timika, Indonesia
    J Infect Dis 204:1613-9. 2011
    ..The epidemiology of congenital malaria was investigated in a hospital-based malaria surveillance study in Papua, Indonesia...
  88. ncbi A randomized intervention of montelukast for post-bronchiolitis: effect on eosinophil degranulation
    Chang Keun Kim
    Department of Pediatrics and Asthma and Allergy Center, Inje University Sanggye Paik Hospital, Seoul, Korea
    J Pediatr 156:749-54. 2010
    ..To investigate the effect of montelukast on eosinophil degranulation and recurrent wheezing episodes in post-respiratory syncytial virus (RSV) bronchiolitis...
  89. pmc Targeting neonatal ischemic brain injury with a pentapeptide-based irreversible caspase inhibitor
    D Chauvier
    Theraptosis Research Laboratory, THERAPTOSIS SA, Pasteur Biotop, Institut Pasteur, Paris 75015, France
    Cell Death Dis 2:e203. 2011
    ..Safety pharmacology investigations, and toxicology studies in rodent and canine neonates, suggest that TRP601 is a lead compound for further drug development to treat ischemic brain damage in human newborns...
  90. ncbi Fluorescence intercalator displacement assay for screening G4 ligands towards a variety of G-quadruplex structures
    Phong Lan Thao Tran
    University of Bordeaux, ARNA Laboratory, Bordeaux, France
    Biochimie 93:1288-96. 2011
    ..Most compounds showed a good G4 vs duplex selectivity but exhibited little, if any, specificity for one quadruplex sequence over the others. The quest for the "perfect" specific G4 ligand is not over yet!..
  91. pmc A chemotype that inhibits three unrelated pathogenic targets: the botulinum neurotoxin serotype A light chain, P. falciparum malaria, and the Ebola filovirus
    Igor Opsenica
    Faculty of Chemistry, University of Belgrade, Studentski trg 16, PO Box 51, 11158 Belgrade, Serbia
    J Med Chem 54:1157-69. 2011
    ..Finally, the 1,7-DAAC-based derivatives were examined for Ebola filovirus inhibition in an assay employing Vero76 cells, and three provided promising antiviral activities and acceptably low toxicities...
  92. ncbi Drug-drug interactions with statins: will pitavastatin overcome the statins' Achilles' heel?
    Alberto Corsini
    Department of Pharmacological Sciences, University of Milan, Italy
    Curr Med Res Opin 27:1551-62. 2011
    ....
  93. pmc A pharmacodynamic study of docetaxel in combination with the P-glycoprotein antagonist tariquidar (XR9576) in patients with lung, ovarian, and cervical cancer
    Ronan J Kelly
    Medical Oncology Branch, Center for Cancer Research, National Cancer Institute, Bethesda, Maryland 20892, USA
    Clin Cancer Res 17:569-80. 2011
    ..Here we report the results of a pharmacokinetic and pharmacodynamic trial using a third-generation, potent, noncompetitive inhibitor of Pgp, tariquidar (XR9576), in combination with docetaxel...
  94. pmc Piperaquine resistance is associated with a copy number variation on chromosome 5 in drug-pressured Plasmodium falciparum parasites
    Richard T Eastman
    Department of Microbiology and Immunology, Columbia University Medical Center, New York, NY 10032, USA
    Antimicrob Agents Chemother 55:3908-16. 2011
    ..Transgene expression studies are underway with individual genes in this segment to evaluate their contribution to piperaquine resistance...
  95. pmc Pharmacokinetics of dihydroartemisinin and piperaquine in pregnant and nonpregnant women with uncomplicated falciparum malaria
    Marcus J Rijken
    Shoklo Malaria Research Unit, PO Box 46 Mae Sot, Tak 63110, Thailand
    Antimicrob Agents Chemother 55:5500-6. 2011
    ..However, a more detailed analysis using population pharmacokinetic modeling is needed to fully investigate the differences found for some of the pharmacokinetic parameters, such as the terminal half-life...
  96. pmc In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1
    Leah Mwai
    Kenya Medical Research Institute KEMRI Wellcome Trust Collaborative Research Program, Kilifi, Kenya
    Antimicrob Agents Chemother 53:5069-73. 2009
    ..Therefore, the use of LM-artemether is likely to lead to the selection of more CQ-susceptible parasites...
  97. pmc Pharmacokinetics and bioequivalence evaluation of two fixed-dose tablet formulations of dihydroartemisinin and piperaquine in Vietnamese subjects
    Nguyen Trong Chinh
    Department of Infectious Diseases, Military Hospital, Hanoi, Vietnam
    Antimicrob Agents Chemother 53:828-31. 2009
    ....
  98. ncbi Pitavastatin inhibits azoxymethane-induced colonic preneoplastic lesions in C57BL/KsJ-db/db obese mice
    Yoichi Yasuda
    Department of Internal Medicine, Gifu University Graduate School of Medicine, Gifu, Japan
    Cancer Sci 101:1701-7. 2010
    ..Therefore, some types of statins, including pitavastatin, may be a useful chemoprevention modality for colon cancer in obese individuals...
  99. pmc Mapracorat, a novel selective glucocorticoid receptor agonist, inhibits hyperosmolar-induced cytokine release and MAPK pathways in human corneal epithelial cells
    Megan E Cavet
    Pharmaceutical R and D, Bausch and Lomb, Inc, Rochester, NY 14609, USA
    Mol Vis 16:1791-800. 2010
    ..This study assessed the anti-inflammatory effects of mapracorat in an in vitro osmotic stress model which mimics some of the pathophysiological changes seen in dry eye...
  100. pmc Should moxifloxacin be used for the treatment of extensively drug-resistant tuberculosis? An answer from a murine model
    Julien Poissy
    Laboratoire de Bacteriologie Hygiene, Faculte de Medecine, Pierre et Marie Curie Université Paris, 91 Boulevard de l Hopital, Paris Cedex 13, France
    Antimicrob Agents Chemother 54:4765-71. 2010
    ....
  101. pmc Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam
    Dao Van Hoang Nguyen
    Department of Infectious Diseases, Military Hospital 175, Ho Chi Minh City, Vietnam
    Antimicrob Agents Chemother 53:3534-7. 2009
    ..Dihydroartemisinin is responsible for most of the ex vivo antimalarial activity of dihydroartemisinin-piperaquine...

Research Grants64

  1. Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout Screening
    RICHARD LAROCK; Fiscal Year: 2009
    ..chromones, benzothiophenes, benzoselenophenes, phthalides, isocoumarins, isochromenes, isoquinolines, quinolines, furans, isoxazoles and various spirotrienones...
  2. Development of a Chloroquine Replacement Drug
    MICHAEL KEVIN RISCOE; Fiscal Year: 2010
    ..emergence and spread of strains of Plasmodium parasites that harbor resistance to multiple drugs including: the quinolines - chloroquine, quinine, and mefloquine;the antifolates - pyrimethamine and sulfadoxine;and the anti-respiratory ..
  3. Discovery of 4-aminoquinoline therapeutics for visceral leishmaniasis
    Peter C Melby; Fiscal Year: 2010
    ..of extensive data related to structure-activity relationship (SAR) and the prior successful development of quinolines for malaria will greatly facilitate the proposed studies...
  4. Increasing efficacy of antineoplastic drugs with gap junction enhancers
    Thu Annelise Nguyen; Fiscal Year: 2010
    ..Recently, we synthesized a new class of substituted quinolines (code name: PQ) and found that they possess potent inhibitory activities against T47D breast cancer cells (IC50 ..
  5. Synthesis of Medicinally Important Heterocycles
    RICHARD LAROCK; Fiscal Year: 2007
    ..chromones and heteroatom analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, naphthols, and phenols...
  6. Phase II Environmentally greener, efficient, and safe synthetic platform for the
    PAUL MATTHEW HERRINTON; Fiscal Year: 2011
    ..Expand the portfolio of borylated pyridine derivatives and add quinolines, pyrazines, pyrimidines, diazenes, imidazoles, pyrazoles, oxazoles, etc. Produce oxidized products (e.g...
  7. NUCLEIC ACID PROBES OF RIBOSOMAL STRUCTURE AND FUNCTION
    BARRY COOPERMAN; Fiscal Year: 2003
    ..Interest in these ribosomal antibiotics has been growing as bacterial resistance to beta-lactams and quinolines has become more widespread...
  8. NOVEL PALLADIUM CATALYZED SYNTHESES OF INDOLE ALKALOIDS
    BJORN SODERBERG; Fiscal Year: 2001
    ..indole-3-acetonitriles, tryptamines, beta-carbolines, 1,2,3,4-tetrahydro-beta-carbolines, pyrrolo[4,3,2-de]quinolines, and pyrrolo[3,2d]indoles will be pursued...
  9. Development of Antimalarial Preclinical Candidates
    Rodney Kiplin Guy; Fiscal Year: 2011
    ..As a back up strategy, the program also targets compounds with the same mechanism of action as existing quinolines. The research design and methods for achieving these goals involves the use of parallel medicinal chemistry;in ..
  10. STRUCTURE SELECTIVITY RELATIONSHIPS OF ANTIBACTERIAL AGE
    CYNTHIA SELASSIE; Fiscal Year: 1992
    ..will encompass two classes of compounds such as 2,4-dihydroxy-5-bromo-7-(methyl-(2,4-diamino-pyrimidinyl)-quinolines Ia and 2,4-diamino-5-(3'-bromo, 4'-carboxamidomethoxy, 5'-acylamino-benzyl) pyrimidine IIb...
  11. Zinc Metabolism in Plasmodium Falciparum
    Oluwatosin Gisanrin; Fiscal Year: 2005
    ..The widely used quinolines and artemisinin classes of antimalarials interfere with metal metabolism to kill the malaria parasite, ..
  12. Novel Reactions of Arynes and their Application to the Synthesis of Anti-Cancer A
    KEITH MEAD; Fiscal Year: 2009
    ..In the event that enimines prove to be superior agents for trapping arynes, the synthesis of 2-aryl-substituted quinolines, 4-quinolones, and quinolinequinones from quinolinium salts will take priority...
  13. QUINOLINES AND CARBAZOLES: MUTAGENS AND CARCINOGENS
    EDMOND LAVOIE; Fiscal Year: 1993
    ..typhimurium and extensive adduct formation has been observed after incubation of 9-acetoxycarbazole with DNA using the 32P-postlabeling technique. We will determine the extent to which similar adducts are formed in vivo in mouse liver...
  14. STUDY OF TYPICAL & ATYPICAL DOPAMINERGIC COMPOUNDS
    Mark Froimowitz; Fiscal Year: 1992
    ..A second aspect of this proposal is the synthesis of derivatives of octohydrobenzo (f) quinolines. The expectation is that one enantiomer of these compounds will be a superpotent dopamine agonist whereas the ..
  15. Novel Anti-Malarials by Combinatorial Pharmacogenomics
    Joseph DeRisi; Fiscal Year: 2006
    ..and Stanford Research Institute (SRI), Inc. Quinolines have a long and rich history of anti-malarial use, yet the diversity of tested compounds to date has been ..
  16. MELANOMA DELINEATING RADIOPHARMACEUTICALS
    Ned Heindel; Fiscal Year: 1980
    Several families of potentially melanophilic radiopharmaceuticals (based on quinolines, psoralens, and melatonin) have been proposed for synthesis, in vitro melanin binding studies, and tumor uptake measurements in animal melanoma models...
  17. Plasmodium Falciparum Metal Metabolism
    David Sullivan; Fiscal Year: 2009
    Interference with Plasmodium metal metabolism by the quinolines and artemisinins is a proven chemotherapeutic target...
  18. MOLECULAR BASIS OF HIGH DENSITY LIPOPROTEIN DEFICIENCY
    ERNST SCHAEFER; Fiscal Year: 2009
    ..The results of this work will provide important insight into the contribution of allelic variation in the pathways of HDL metabolism, inflammation, and insulin resistance to the complex phenotype of low HDL-C. ..
  19. Targeting of the Androgen Receptor in Prostate Cancer
    John Isaacs; Fiscal Year: 2005
    ..These peptide prodrugs will be designed so that they are substrates for the enzymatic activity of either Prostate Specific Antigen. ..
  20. THE PHYSIOLOGY OF DRUG RESISTANT MALARIA
    PAUL ROEPE; Fiscal Year: 2009
    ..Knowledge gained during this research will significantly expand our understanding of malarial parasite physiology and antimalarial drug resistance. ..
  21. Pharmacogenetics of the Statin Response
    ERNST SCHAEFER; Fiscal Year: 2006
    ..These results can be used to formulate guidelines for identifying elderly subjects for statin treatment to prevent future CHD. ..
  22. Interest of IKr-related Abnormalities of ECGs to Improve Drug-safety Evaluation
    Jean Philippe Couderc; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  23. Defining Moxifloxacin as a First-line TB Drug
    Eric Nuermberger; Fiscal Year: 2008
    ..Relevance: Results of these studies will help to define optimal treatment regimens for TB that can be used to design new clinical trials or, in some cases, directly applied to clinical practice. ..
  24. Dysfunctional Telomeres, Checkpoints and Aging
    KWOK KIN WONG; Fiscal Year: 2010
    ....
  25. DIETARY COMPOSITION, OBESITY, AND CARDIOVASCULAR RISK
    ERNST SCHAEFER; Fiscal Year: 2003
    ..abstract_text> ..
  26. CARE Network - Madison Clinical Center
    ROBERT LEMANSKE; Fiscal Year: 2008
    ..abstract_text> ..
  27. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  28. WGA Study to Identify Genetic Variants Associated with CV Events in CHS
    Bruce Psaty; Fiscal Year: 2009
    ..The proposed three-part study is efficient, has excellent power to detect small to modest-sized hazard ratios, provides a large sample of WG scans for aim 2, and includes an external replication. (End of Abstract) ..
  29. Inhibition of Alzheimer's Beta-Amyloid Fibril Formation
    Duy Hua; Fiscal Year: 2009
    ..However, soluble oligomeric Abeta showed high neuronal toxicity. Inhibition of the formation of these toxic soluble Abeta oligomers would provide therapeutics for AD. ..
  30. Glycine Transport Inhibition for Nicotine Dependence in Schizophrenia
    A Evins; Fiscal Year: 2009
    ....
  31. Innate Immunity and exacerbations of COPD
    Sanjay Sethi; Fiscal Year: 2009
    ..The overall goal of this research is to identify specific aspects of the innate defense of the lung that determine the frequency of exacerbations in COPD that will serve as potential therapeutic targets to reduce exacerbations. ..
  32. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  33. Smoking Cessation and Smoking Relapse Prevention in Patients with Schizophrenia
    A Eden Evins; Fiscal Year: 2010
    ..Participants will then discontinue study medications and enter a 3-month follow up. The primary outcome measure will be 7-day point prevalence abstinence rate at 12 months in the intervention vs. placebo groups. ..
  34. Artificial Cornea Based on Photolithographically Patterned, Biomimetic Hydrogels
    Christopher N Ta; Fiscal Year: 2010
    ..3. Determine the skirt design for optimal stromal tissue integration by evaluating in vitro and in vivo stromal wound healing within photolithographically patterned, microperforated hydrogel arrays. ..
  35. Deciphering synergistic combinatorial targets in glioma
    W K Alfred Yung; Fiscal Year: 2010
    ....
  36. Macrophage Foam Cells, Cathepsins and Cholesterol Efflux
    ALAN RICHARD TALL; Fiscal Year: 2010
    ..These mechanistic insights may suggest new treatments for vulnerable human plaques such as LXR activators, CatK inhibitors or inhibitors of RANK signaling. ..
  37. Cross-Coupling Reactions of Organosilanols
    SCOTT DENMARK; Fiscal Year: 2009
    ..Synthetic approaches to isodomoic acid H, hepatitis C viral inihibiting indole alkaloids, the salicylihalimide macrolactone oximidine II, and polyene antiviral antibiotic viridenomycin are detailed. ..
  38. Clinical Trial of Acid Reflux Therapy in Asthma
    Robert Wise; Fiscal Year: 2007
    ..Pre-specified subgroup analyses will be conducted to determine if there are clinical or demographic characteristics that predict benefit from treatment of GERD in asthma. ..
  39. Effects of Massage on Immune System of Preterm Infants
    Jocelyn Ang; Fiscal Year: 2007
    ..Data from this study could also impact future explorations on potential effects of MT on the immune responses to childhood vaccinations and susceptibility to bacterial and viral infections. [unreadable] [unreadable]..
  40. Atherogenic Effects of Tyrosine Oxidation in HDL
    John Oram; Fiscal Year: 2004
    ....
  41. ANTIHYPERTENSIVE DRUG/GENE INTERACTIONS AND CV EVENTS
    Bruce Psaty; Fiscal Year: 2004
    ..58 (the difference between an odds ratio of 0.46 and 0.79 in subjects with and without the variant, respectively). Power for other primary aims is excellent; power for secondary aims is good to excellent. ..
  42. C. difficile Toxin Membrane Test with Magnetic Particles
    ROBERT CARMAN; Fiscal Year: 2004
    ..perfringens enterotoxin, another cause of AAD. The technology developed in this project will be widely applicable for the development of new highly sensitive stool antigen tests. ..
  43. Trends in and Outcomes of Medication Use in Older Adults
    Bruce Psaty; Fiscal Year: 2004
    ..abstract_text> ..
  44. Mycobacterium tuberculosis cell wall virulence factors
    Susan Dorman; Fiscal Year: 2004
    ..Finally, new information from the proposed self-contained pilot studies will serve as the foundation for future comprehensive dissection of macrophage response pathways affected by specific cell wall components. ..
  45. REGULATION OF NEUTROPHIL OXIDATIVE RESPONSES IN TRAUMA
    Joseph Solomkin; Fiscal Year: 2004
    ..Together, these studies will define potential points for therapeutic intervention and provide important insight into regulation of the acute inflammatory response. ..
  46. ASTHMA AND INTERVENTIONS IN THE EMERGENCY DEPARTMENT
    Robert Strunk; Fiscal Year: 2002
    ..The intent to treat model will be used, as primary outcome can be obtained after consent even if not contact cannot be made at 2 week and 6 month phone calls. ..
  47. Postprandial Lipemia and Endothelial Function In ACCORD
    Henry Ginsberg; Fiscal Year: 2004
    ....
  48. Narp Expression and Drugs of Abuse
    Irving Reti; Fiscal Year: 2002
    ..B) Develop methods to manipulate expression of Narp in the VTA using the herpes simplex virus vector system. ..
  49. BIOCHEMISTRY OF PROTEIN PRENYLATION
    Michael Gelb; Fiscal Year: 2002
    ....
  50. SCAVENGER RECEPTOR B1 AND HDL METABOLISM
    Alan Tall; Fiscal Year: 2005
    ..The work will provide crucial insights into the cellular mechanisms underlying the final step of reverse cholesterol transport. The findings will be relevant to the relationship between HDL, atherosclerosis and gallstone formation. ..
  51. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
    ..abstract_text> ..
  52. Chemical and Biological Studies on Biaryl Phenolics
    Ken Feldman; Fiscal Year: 2005
    ..The search for selective 20S proteosome inhibitors among the Ntn-type proteases will be advanced by these investigations. ..
  53. Role of Inter-alpha Inhibitors in Anthrax Intoxication
    Steven Opal; Fiscal Year: 2007
    ..Our research is focused on the development of a new and safe treatment based on the ability of inter-alpha proteins to prevent the fatal consequences of anthrax infection. [unreadable] [unreadable] [unreadable] [unreadable]..
  54. Rapid Detection of Mycobacterium tuberculosis
    Susan Dorman; Fiscal Year: 2007
    ..unreadable] [unreadable] Relevance: Results of these studies will improve our understanding of the laboratory performance and clinical benefit of this test, and lead to improved detection and treatment of TB. [unreadable] [unreadable]..
  55. Poly(ADP-ribose) polymerase in diabetic nephropathy
    IRINA OBROSOVA; Fiscal Year: 2006
    ..abstract_text> ..
  56. Pharmacogenetics and Cardiovascular Events
    Bruce Psaty; Fiscal Year: 2006
    ..The primary defense is replication: we would therefore welcome collaboration from others in the Pharmacogenetics Network in validation efforts. ..
  57. Neural Analysis of Maternal Aggression
    STEPHEN GAMMIE; Fiscal Year: 2006
    ..Basic research into sex differences in aggression, then, is important to understanding the biological underpinnings of sex and gender differences in social behavior, health, and disease. ..
  58. Glutamate Vesicular Transport:Pharmacophore Development
    Charles Thompson; Fiscal Year: 2006
    ..Using N-term VGLUT antibodies, affinity tags, tethered- and cross-linking probes, VGLUT residues and structures proximal to VGLUT will be isolated and identified by mass spectrometry. ..
  59. Novel Pathways of Cellular Cholesterol Efflux
    Alan Tall; Fiscal Year: 2005
    ....
  60. A proteomics approach in the study of novel COPD markers
    Ratko Djukanovic; Fiscal Year: 2005
    ..Finally, applying the antibodies to archival lung tissue samples we will be able to localize the COPD-selective proteins to the airway and alveoli, adding valuable knowledge to our understanding of COPD mechanisms. ..
  61. ASTHMA CLINICAL RESEARCH NETWORK
    ROBERT LEMANSKE; Fiscal Year: 2002
    ....
  62. Prospective Study of Diet, Physical Activity, BMI and Risk of Pulmonary Embolism
    Carlos Camargo; Fiscal Year: 2008
    ..We believe that quantifying these modifiable risk factors will lead to public health interventions that decrease the incidence of pulmonary embolism in the elderly population. [unreadable] [unreadable] [unreadable]..
  63. Triple Anti-Angiogenic Therapy for Brain Tumors
    W K Yung; Fiscal Year: 2007
    ..abstract_text> ..